DC Chemicals supplies: RG108,cas: 48208-26-0,Catalog: DC7584,In stock.
Contact: website:www.dcchemicals.com,
sales@dcchemicals.com,order@dcchemicals.com,info@dcchemicals.com,
Tel: +86-21-58447131;Fax:+86-21-61643258；
Product name: RG108, Synonyms: , cas: 48208-26-0, MW: 334.33, Molecule Formula: C19H14N2O4
RG108, cas 48208-26-0, Purity>98%. Best price and quality from DC Chemicals. This orally available drug is an antagonist of the serotonin 6 (5-HT6) receptor. This receptor subtype is expressed primarily in the brain, particularly in the cerebral cortex and hippocampus, where it has been proposed to play a role in cognitive impairments associated with schizophrenia and Alzheimer's disease. The 5-HT6 receptor antagonists are thought to enhance cholinergic, glutamatergic, noradrenergic, and dopaminergic neurotransmission. Apart from some affinity for adrenergic receptors, Lu AE58054 has been reported to be highly selective over other G-protein coupled receptors. The compound enters the brain and dose-dependently reversed deficits in a rat model of cognitive impairment (Upton et al., 2008; Arnt et al., 2010). Lu AE58054 is being developed as a symptomatic adjunct to cholinesterase inhibitor treatment in Alzheimer's disease. Lu AE58054 was originally discovered by Lilly, which licensed it to the biotechnology company Saegis for the development of cognitive impairment in thinking disorders such as schizophrenia. In 2006, Saegis was acquired by Lundbeck, which in October 2013 launched a global Phase 3 program in AD. This program consists of four trials planned to enroll a total of about 3,000 patients (see company press release).
RG108 effectively blocks DNA methyltransferases in vitro and does not cause covalent enzyme trapping in human cell lines. Incubation of cells with low micromolar concentrations of RG108 results in significant demethylation of genomic DNA without any detectable toxicity. Intriguingly, RG108 causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences. [1] In another study, the synthesis and in vitro analysis of a biotinylated RG108 conjugate is investigated to evaluate the interactions with DNA methyltransferase enzymes. [2] In a recent study, it is shown RG108 can significantly reduce the DNA methyltransferases activity in SM derived iPS cells as compared to the native SMs. [3]For the detailed information of RG108, the solubility of RG108 in water, the solubility of RG108 in DMSO, the solubility of RG108 in PBS buffer, the animal experiment (test) of RG108, the cell expriment (test) of RG108, the in vivo, in vitro and clinical trial test of RG108, the EC50, IC50,and Affinity of RG108, Please contact DC Chemicals.
没有评论:
发表评论